Therapeutic modulation of retinoid X receptors – SAR and therapeutic potential of RXR ligands and recent patents

Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype

(2019) Pascal Heitel et al.   ACS Medicinal Chemistry Letters

Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation

(2019) Julius Pollinger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Alternative retinoid X receptor (RXR) ligands

(2019) Wojciech Krężel et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Emerging roles of bexarotene in the prevention, treatment and anti-drug resistance of cancers

(2018) Danyang Shen et al.   Expert Review of Anticancer Therapy

Computer-Assisted Discovery of Retinoid X Receptor Modulating Natural Products and Isofunctional Mimetics

(2018) Daniel Merk et al.   JOURNAL OF MEDICINAL CHEMISTRY

Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery

(2017) Ewgenij Proschak et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nurr1:RXRα heterodimer activation as monotherapy for Parkinson’s disease

(2017) Athanasios D. Spathis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

An Endogenous Mammalian Retinoid X Receptor Ligand, At Last!

(2016) Ángel R. de Lera et al.   ChemMedChem

Preventive and Therapeutic Effects of the Retinoid X Receptor Agonist Bexarotene on Tumors

(2016) Lisi Qi et al.   CURRENT DRUG METABOLISM

Double-blind, placebo-controlled, proof-of-concept trial of bexarotene in moderate Alzheimer’s disease

(2016) Jeffrey L. Cummings et al.   Alzheimers Research & Therapy

Nitrostyrene Derivatives Act as RXR  Ligands to Inhibit TNF  Activation of NF- B

(2015) Z. Zeng et al.   CANCER RESEARCH

Chances and challenges of retinoid X receptor gamma targeting for regenerative multiple sclerosis treatment

(2015) Daniel Merk   Future Medicinal Chemistry

Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers

(2015) Venkatram R. Atigadda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nuclear receptor full-length architectures: confronting myth and illusion with high resolution

(2015) Fraydoon Rastinejad et al.   TRENDS IN BIOCHEMICAL SCIENCES

Effect of NKG2D ligand expression on host immune responses

(2015) Marine Champsaur et al.   IMMUNOLOGICAL REVIEWS

Retinoid X receptor ligands: a patent review (2007 – 2013)

(2014) Shoya Yamada et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Methyl Substitution of a Rexinoid Agonist Improves Potency and Reveals Site of Lipid Toxicity

(2014) Venkatram R. Atigadda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Functions, Therapeutic Applications, and Synthesis of Retinoids and Carotenoids

(2013) Rosana Álvarez et al.   CHEMICAL REVIEWS

Defining the Communication between Agonist and Coactivator Binding in the Retinoid X Receptor α Ligand Binding Domain

(2013) LeeAnn J. Boerma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Modeling, Synthesis, and Biological Evaluation of Potential Retinoid X Receptor (RXR) Selective Agonists: Novel Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic Acid (CD3254)

(2013) Peter W. Jurutka et al.   JOURNAL OF MEDICINAL CHEMISTRY

ApoE-Directed Therapeutics Rapidly Clear  -Amyloid and Reverse Deficits in AD Mouse Models

(2012) P. E. Cramer et al.   SCIENCE

Current advances in the treatment of Alzheimer's disease: focused on considerations targeting Aβ and tau

(2012) Yang Hong-Qi et al.   Translational Neurodegeneration

Modulation of RXR function through ligand design

(2011) Efrén Pérez et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Structure Basis of Bigelovin as a Selective RXR Agonist with a Distinct Binding Mode

(2011) Haitao Zhang et al.   JOURNAL OF MOLECULAR BIOLOGY

Molecular Determinants of Magnolol Targeting Both RXRα and PPARγ

(2011) Haitao Zhang et al.   PLoS One

Danthron Functions as a Retinoic X Receptor Antagonist by Stabilizing Tetramers of the Receptor

(2010) Haitao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of a Naturally Occurring Rexinoid, Honokiol, That Activates the Retinoid X Receptor

(2010) Hitoshi Kotani et al.   JOURNAL OF NATURAL PRODUCTS

Retinoid X receptor gamma signaling accelerates CNS remyelination

(2010) Jeffrey K Huang et al.   NATURE NEUROSCIENCE

Modulating Retinoid X Receptor with a Series of (E)-3-[4-Hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic Acids and Their 4-Alkoxy Isomers†

(2009) Efrén Pérez Santín et al.   JOURNAL OF MEDICINAL CHEMISTRY

Modeling, Synthesis and Biological Evaluation of Potential Retinoid X Receptor (RXR) Selective Agonists: Novel Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene)

(2009) Carl E. Wagner et al.   JOURNAL OF MEDICINAL CHEMISTRY

The First Potent Subtype-Selective Retinoid X Receptor (RXR) Agonist Possessing a 3-Isopropoxy-4-isopropylphenylamino Moiety, NEt-3IP (RXRα/β-dual agonist)

(2008) Kayo Takamatsu et al.   ChemMedChem

Pathophysiology, Clinical Presentation, and Management of Colon Cancer

(2008) Mitchell S. Cappell   GASTROENTEROLOGY CLINICS OF NORTH AMERICA

NKG2D ligands: key targets of the immune response

(2008) Segundo González et al.   TRENDS IN IMMUNOLOGY